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Updated: Sep 13, 2026

Differential Effects of Lipid-lowering Drugs in Modulating Morphology of Cholesterol Particles
Published on: November 10, 2017
[Trends toward development of other novel antihyperlipidemic drugs]
1Department of Internal Medicine and Molecular Science, Graduate School of Medicine, Osaka University.
Insights
Statins reduce cardiac events, but some hyperlipidemia is resistant to treatment. Novel antihyperlipidemic drugs are being developed to inhibit or reverse atherosclerosis progression.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
Context:
- HMG-CoA reductase inhibitors (statins) are used for primary and secondary prevention of cardiac events.
- Conventional antihyperlipidemic drugs do not completely prevent cardiac events.
- Some patients exhibit hyperlipidemia resistant to standard treatments.
- Regression of atherosclerosis remains challenging even with normolipidemia post-treatment.
Purpose:
- To review novel antihyperlipidemic drugs under development.
- To explore mechanisms beyond statins for managing hyperlipidemia and atherosclerosis.
Summary:
- The review discusses emerging antihyperlipidemic drug classes targeting novel mechanisms.
- These include inhibitors of cholesterol synthesis (squalene synthase, squalene epoxidase).
- Ileal Na+/bile acid cotransporter (IBAT) inhibitors and intestinal cholesterol absorption inhibitors are also covered.
Impact:
- These novel agents are expected to inhibit atherosclerosis progression or induce regression in clinical settings.
- They offer potential therapeutic options for patients with statin-resistant hyperlipidemia.
- Advancements may improve management of atherosclerosis beyond current lipid-lowering strategies.
Abstract:
A number of primary and secondary prevention studies with HMG-CoA reductase inhibitors(statins) have shown a reduction of cardiac events. However, such cardiac events cannot be completely prevented by antihyperlipidemic drugs there are a number of patients whose hyperlipidemia is resistant to conventional treatment. Furthermore, it is still difficult to observe a regression of atherosclerosis even when patients become normolipidemic after treatment. Thus, many antihyperlipidemic drugs with novel mechanisms are under development and are expected to inhibit progression or rather obtain regression of atherosclerosis in clinical settings. In the current review, inhibitors of cholesterol synthesis such as squalene synthase and squalene epoxidase inhibitors, ileal Na+/bile acid cotransporter(IBAT) inhibitors, and inhibitors of intestinal cholesterol absorption are described.
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